Prevention and Treatment of Thromboembolic Disorders

• US 20090004265A1
• Filed: 01/19/2006
• Published: 01/01/2009
• Est. Priority Date: 01/31/2005
• Status: Active Grant

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer Healthcare AG (Bayer AG)
• Inventors: Park, Son-Mi, Wehling, Klaus, Kubitza, Dagmar, Misselwitz, Frank
• Granted Patent: US 9,539,218 B2
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/5377 not condensed and containing further heterocyclic rings, e.g. timolol
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention relates to the field of blood coagulation, more specifically it relates to a method of treating a thromboembolic disorder by administering once daily a direct factor Xa inhibitor in oral dosage form to a patient in need thereof, wherein the factor Xa inhibitor has a plasma concentration half life indicative of a bid or tid administration interval, e.g. of 10 hours or less.

Claims

1. A method of treating a thromboembolic disorder comprising administering a direct factor Xa inhibitor no more than once daily for at least five consecutive days in an oral dosage form to a patient in need thereof, wherein said inhibitor has a plasma concentration half life of 10 hours or less when orally administered to a human patient.

2. The method of claim 1, wherein one dosage form is administered.

4. The method or use as claimed in any of claims 1 to 3, wherein the thromboembolic disorder is ST Segment Elevation Myocardial Infarction (STEMI), Non ST Segment Elevation Myocardial Infarction (NSTEMI), unstable angina, reocclusion after angioplasty or aortocoronary bypass, pulmonary embolisms, deep vein thromboses or stroke.

5. The method or use as claimed in any of claims 1 to 4, wherein the oral dosage form is a rapid-release tablet.

6. The method or use as claimed in any of claims 1 to 5, wherein the direct factor Xa inhibitor is 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide.

3. The use of an oral dosage form of a direct factor Xa inhibitor for the manufacture of a medicament for the treatment of a thromboembolic disorder administered once daily for at least five consecutive days, wherein said inhibitor has a plasma concentration half life of 10 hours or less when orally administered to a human patient.

7. A packaged pharmaceutical composition comprising a container containing a rapid-release tablet comprising 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, said container furthermore containing instructions for using said rapid-release tablet to treat a thromboembolic disorder.

8. The packaged pharmaceutical composition of claim 7, comprising a container containing a rapid-release tablet comprising 5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, said container furthermore containing instructions for administering said rapid-release tablet at a frequency of once daily.